Background: The safe and efficient delivery of chemotherapeutic agents is critical to glioma therapy. However, chemotherapy for glioma is extremely challenging because the blood–brain barrier (BBB) rigorously prevents drugs from reaching the tumor region.
Materials and Methods: TfR-T12 peptide-modified PEG-PLA polymer was synthesized to deliver paclitaxel (PTX) for glioma therapy. TfR was significantly expressed on brain capillary endothelial cells and glioma cells; therefore, TfR-T12 peptide-modified micelles can cross the BBB system and target glioma cells.
Results: TfR-T12-PEG-PLA/PTX polymeric micelles (TfR-T12-PMs) could be absorbed rapidly by tumor cells, and traversed effectively the BBB monolayers. TfR-T12-PMs can effectively inhibit the proliferation of U87MG cells in vitro, and TfR-T12-PMs loaded with paclitaxel presented better antiglioma effect with prolonged median survival of nude mice-bearing glioma than the unmodified PMs.
Conclusion: The TfR-T12-PMs could effectively overcome the BBB barrier and accomplish glioma-targeted drug delivery, thus validating its potential in improving the therapeutic outcome in multiforme.



中文翻译：

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转铁蛋白受体靶向 PEG-PLA 聚合物胶束用于多形性胶质母细胞瘤的化疗

背景：化疗药物的安全和有效递送对于胶质瘤治疗至关重要。然而，胶质瘤的化疗极具挑战性，因为血脑屏障 (BBB) 严格阻止药物到达肿瘤区域。
材料和方法：合成了 TfR-T12 肽修饰的 PEG-PLA 聚合物，以提供紫杉醇 (PTX) 用于胶质瘤治疗。TfR在脑毛细血管内皮细胞和胶质瘤细胞上显着表达；因此，TfR-T12 肽修饰的胶束可以穿过 BBB 系统并靶向胶质瘤细胞。
结果：TfR-T12-PEG-PLA/PTX聚合物胶束（TfR-T12-PMs）可以被肿瘤细胞迅速吸收，并有效地穿过BBB单层。TfR-T12-PMs在体外能有效抑制U87MG细胞的增殖，与未修饰的PMs相比，载有紫杉醇的TfR-T12-PMs表现出更好的抗神经胶质瘤作用，延长了荷荷裸鼠胶质瘤的中位生存期。
结论： TfR-T12-PMs可有效克服BBB屏障，实现胶质瘤靶向给药，从而验证其在改善多形性肿瘤治疗结果方面的潜力。